Catalog Number: 5683
Chemical Name: N-Methyl-L-valyl-N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide
Biological Activity
Potent, synthetic, cytotoxic analog of dolastatin 10 (Cat. No. 3375). Suppresses tumor cell viability in vitro (GIC50 values are 0.22, 0.49 and 0.54 nM in BT474, MDA-MB-361-DYT2 and N87 cells, respectively). MMAE derivatives have been shown to induce regression of established tumor xenografts when conjugated to tumor targeting antibodies via a protease-cleavable linker.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at -20°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Development of potent monoclonal antibody auristatin conjugates for cancer therapy.
    Doronina et al.
    Nat.Biotechnol., 2003;21:778
  2. Discovery of cytotoxic dolastatin 10 analogues with N-terminal modifications.
    Maderna et al.
    J.Med.Chem., 2014;57:10527
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